Alsterpaullone Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, reported to be the most active paullone.

Alsterpaullone  (CAS 237430-03-4)

Alsterpaullone is rated 5.0 out of 5 by 1.
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| See 1 Citations
Synonym: 9-Nitropaullone
Application: A potent ATP-competitive and cell cycle cylin-dependent kinase inhibitor
CAS Number: 237430-03-4
Purity: >95%
Molecular Weight: 293.28
Molecular Formula: C16H11N3O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
Alsterpaullone sc-202453 1 mg $60.00
Alsterpaullone sc-202453A 5 mg $294.00

Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone (sc-208152). The paullones belong to a family of benzazepinones, and are described to highly inhibit neuronal CDK5/p25 and glycogen synthase kinase-3β (GSK-3β). Studies report that Alsterpaullone activates caspase-9 and enhances apoptosis in Jurkat cells, inhibits CDK5/p25-dependent phosphorylation of DARPP-32 in in vitro mouse striatum slices, and blocks the phosphorylation of Tau by GSK-3β.


References

1. Leost, M., et al., 2000. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. European journal of biochemistry / FEBS. 267(19): 5983-94. PMID: 10998059
2. Lahusen, Tyler., et al., 2003. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Molecular carcinogenesis. 36(4): 183-94. PMID: 12669310

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (≥10 mg/ml). Insoluble in water, and 100% ethanol.
Storage :
Store at -20° C
Melting Point :
238.72° C (Predicted)
Boiling Point :
651.53° C at 760 mmHg (Predicted)
Density :
1.46 g/cm3 (Predicted)
Refractive Index :
n20D 1.74 (Predicted)
IC50 :
CDK1/cyclin B: IC50 = 35 nM; CDK2/cyclin E: IC50 = 200 nM; CDK5/p25: IC50 = 40 nM; CDK5/p35: IC50 = 40 nM; GSK-3β: IC50 = 4 nM; Glycogen synthase kinase-3 alpha: IC50 = 4 nM (human)
Ki Data :
CDK2: Ki= 80 nM (human); Glycogen synthase kinase 3: Ki= 0.11 µM (human); LCK: Ki= 0.47 µM (human)
pK Values :
pKb: 1.02 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5005498
MDL Number :
MFCD02683579
SMILES :
C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)[N+](=O)[O-]

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Certificate of Analysis

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Citations 1 to 1 of 1 total

PMID: # 10998059
Leost, M. et al. 2000. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur. J. Biochem.. 267: 5983-5994.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Lahusen et al Lahusen et al. (PubMed ID 12669310) found that Alsterpaullone induced apoptosis and promoted loss of clonogenicity in the Jurkat cell line. -SCBT Publication Review
Date published: 2015-06-09
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